Sodium Channel

Procainamide Hydrochloride (Procapan) is the hydrochloride salt form of procainamide, an amide derivative exhibiting class 1A antiarrhythmic property and analog of procaine. Procainamide hydrochloride reversibly binds to and blocks activated (open) voltage-gated sodium channels, thereby blocks the influx of sodium ions into the cell, which leads to an increase in threshold for excitation and inhibit depolarization during phase 0 of the action potential.

Rilmakalim is a potassium channel opener. Rilmakalim shows antivasoconstrictor effect.

Amiloride hydrochloride (Amiloride HCl) is an effective sodium channel blocker of epithelial.

Phenytoin sodium (Diphantoine) is an inactive stabilizer for voltage-gated sodium channel .

λ-Cyhalothrin (Icon) is a type II synthetic pyrethroid insecticide featuring a high-efficiency, broad-spectrum formula with an α-cyano group. It is employed across various applications for controlling a wide array of pests. As a neurotoxin, λ-Cyhalothrin acts on sodium channels in neuron membranes within the central nervous system.

Zoniporide hydrochloride is a selective inhibitor of NHE-1 with IC50 of 14 nM which is >150-fold selectivity versus other NHE isoforms. Zoniporide hydrochloride shows an IC50 of 59 nM for NHE-1-dependent swelling of human platelets.

Mebeverine hydrochloride (Colofac Hydrochloride), a β-phenylethylamine derivative, is a potent α1 repector inhibitor, relaxing the muscles in and around the gut.

Ambroxol hydrochloride (Mucosolvan) is a metabolite of BROMHEXINE that stimulates mucociliary action and clears the air passages in the respiratory tract. It is usually administered as the hydrochloride.

Ropivacaine (LEA-103 HCl) is a local anaesthetic drug belonging to the amino amide group.

Monensin sodium is an antiprotozoal agent produced by Streptomyces cinnamonensis.Monensin sodium salt (Monensin A sodium salt) causes a marked enlargement of the MVBs and regulates exosome secretion

Indazole is also called benzpyrazole or isoindazone. Its derivatives exhibit a wide range of biological activities. Indazole and its derivatives can be used in the research of cancer, neurological diseases, cardiovascular diseases, and gastrointestinal diseases.

L-Aspartic aicd sodium (Sodium L-aspartate) is an amino acid, a precursor active molecule for colon-specific active molecule delivery, that promotes Na+ efflux from rat forebrain membrane vesicles.

(Rac)-AMG8379 ((Rac)-AMG8380) is a racemate of AMG8379 which is an orally active and selective sulfonamide NaV1.7 antagonist.

N-Me-aminopyrimidinone9 is a sodium channel antagonist

SB-237376 HCl (SB-237376 hydrochloride) is a calcium and potassium channel antagonist used in the treatment of cardiac arrhythmias.

Crobenetine (BIII 890 CL) Free Base is a selective NaV channel blocker that eliminates VTD-induced [Ca2+] elevation.

E 0747 (E0747) is a new antiarrhythmic compound that inhibits arrhythmias by inhibiting Na channels in cardiac cells.

Lifarizine FA is a sodium channel blocker used in the treatment of neurological disorders and cardiovascular diseases, study of stroke.

Orphenadrine is a noncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist that inhibits clonal HERG channels in a concentration-dependent manner, producing an IC of 0.85 μM in HEK cells.Orphenadrine is an antagonist of central and peripheral muscarinic receptors. Attenuation is blocked by mutations in pore residues Y652 or F656. Orphenadrine has antispasmodic, analgesic, and anticholinergic activity and protects against glutamatergic neurotoxicity in vitro and in vivo.Orphenadrine has inhibitory effects on sodium channels and can be used in the treatment of Parkinson's disease.

SM-6586 is a potent calcium channel antagonist with inhibitory effects on Na+/H+ and Na+/Ca2+ exchange channels, and can be used in the study of cerebrovascular disease and hypertension, among other diseases.

Besipirdine (HP 749 free base) is a non-receptor-dependent cholinomimetic compound with alpha-adrenergic and cardiovascular activities.Besipirdine inhibits voltage-dependent sodium-potassium channels and inhibits biogenic amine uptake.Besipirdine reduces schedule-induced irritability and thirst and enhances cholinergic and adrenergic activity in the CNS in the rat. Besipirdine reduces schedule-induced thirst and enhances cholinergic and adrenergic neurotransmission in the central nervous system.

PF-05186462 (PF-05150122) is a potent, state-dependent, subtype selective Nav1.7 inhibitor with IC50 of 21 nM, no significant activity against Nav1.5.

(5R)-BW-4030W92 is the R-type of BW-4030W92, the active enantiomer. (5R)-BW-4030W92 is an orally available, non-selective, voltage-dependent and use-dependent sodium channel antagonist for the study of neurological disorders.

Aneratrigine hydrochloride is a sodium channel protein type 9 subunit blocker that may be used for the prevention or treatment of sodium channel blocker-related diseases.

Sulcardine 2HCl is a multi-ion channel blocker with antiarrhythmic effects that blocks the properties of hERG and hNav1.5 channels and can be used to study atrial fibrillation and ventricular arrhythmias.

Benzocaine shares a common receptor with all othe rLAs in the voltage-gated Na+ channel(IC50 of 0.8 mM tested with a potential of +30 mV).

Ralfinamide mesylate (FCE-26742A (mesylate)) is an orally available Na+ channel blocker.

Nav1.8-IN-1 (CHEMBL1270208) is an inhibitor of human NaV1.8

Transcainide(R 54718), a new lidocaine analog, is an orally active antiarrhythmic agent.Transcainide blocks the open state of BTX-activated sodium channels in bovine heart and rat skeletal muscle.

R 56865 is a weak potential-operated channel inhibitor that inhibits the late sodium current in human isolated cardiomyocytes.

Elpetrigine (GW273293) is a potential sodium channel blocker with antiepileptic activity that can be used to study epilepsy.

BIIB 722 Mesylate is a selective sodium-hydrogen exchange inhibitor with cardioprotective properties and can be used to study myocardial ischemia and myocardial infarction.

Raxatrigine (CNV 1014802) has been investigated for the treatment of Bipolar Disorder and Bipolar Depression.

β-Pompilidotoxin Acetate is a wasp venom peptide. β-Pompilidotoxin Acetate can slow sodium channel inactivation and increase steady-state sodium current in cells.

VGSCs-IN-1 is a potent VGSC inhibitor, a 2-piperazine analog of Riluzole that exhibits good blocking activity on Nav1.4.VGSCs-IN-1 can be used to study cellular excitability disorders.

SB-237376 is a calcium and potassium channel antagonist used to treat cardiac arrhythmias.

Bupivacaine hydrochloride monohydrate is a potent NMDA receptor inhibitor of sodium, L-calcium, and potassium channels.Bupivacaine hydrochloride monohydrate inhibits SCN5A channels and is commonly used in the study of chronic pain.

Myomodulin acetate is present in two identified aplysia neurons that contain myomodulin A the ARC motor neuron B16 and the abdominal neuron L10.

KT-362 fumarate is a novel compound that acts as an antagonist of calcium channels, potassium channels and sodium channels.KT-362 fumarate causes vasodilation by affecting intracellular calcium mobilization in atrial muscle cells.KT-362 fumarate has a relaxing effect on femoral and basilar artery strips in rabbits.

Rimeporide hydrochloride (EMD-87580 hydrochloride) is a potent and selective Sodium hydrogen exchange 1 (NHE-1) inhibitor.

5-(N,N-Hexamethylene)-amiloride (5-HMA) is an amiloride derivative, shown to inhibit TRPA1-mediated calcium signal (IC50: 35 μM). It is an inhibitor of the Na+/H+ exchanger (NHE), with Ki of 0.013-2.4 μM for various NHE isoforms. 5-HMA also blocks ASIC3 channels by 51% at 20 μM.

GX-585 is a sulfonamide analog that is a Nav 1.7 channel inhibitor with analgesic activity for the study of neuropathic pain and inflammation.

Sipatrigine (619C89) is an antiepileptic compound with neuroprotective activity through glutamate release, TREK ion channels, TRESK channels, sodium channels, and calcium channel inhibitors in the CNS, and can be used to study TRESK channels.

PF 04531083 is a selective blocker of the NaV1.8 channel. PF 04531083 can be used for neuropathic and inflammatory pain studies.

GX 201 is a selective NaV1.7 inhibitor, IC50 of < 3.2 nM for hNaV1.7.

Lamotrigine (BW430C) is an Anti-epileptic Agent and Mood Stabilizer. The physiologic effect of lamotrigine is by means of Decreased Central Nervous System Disorganized Electrical Activity.

Lidocaine hydrochloride (Lignocaine hydrochloride) is a local anesthetic and cardiac depressant used as an antiarrhythmic agent. Its actions are more intense and its effects more prolonged than those of PROCAINE but its duration of action is shorter than that of BUPIVACAINE or PRILOCAINE.

Halofuginone specifically inhibits collagen type I gene expression and matrix metalloproteinase 2 (MMP-2) gene expression, which may result in the suppression of angiogenesis, tumor stromal cell development, and tumor cell growth. Halofuginone Hydrobromide is the hydrobromide salt of halofuginone, a semisynthetic quinazolinone alkaloid anticoccidial derived from the plant Dichroa febrifuga, with antifibrotic and potential antineoplastic activities. These effects appear to be due to halofuginone-mediated inhibition of the collagen type I and MMP-2 promoters. Collagen type I and MMP-2 play important roles in fibroproliferative diseases.

Zonisamide (AD 810), a sulfonamide anticonvulsant, is approved for use as an adjunctive treatment in adults with partial-onset seizures. It may inhibit a carbonic anhydrase although this is not one of the main mechanisms of action. Zonisamide may act by blocking repetitive firing of voltage-gated sodium channels results in a reduction of T-type calcium channel currents, or by binding allosterically to GABA receptors. This latter action may lower the uptake of the inhibitory neurotransmitter GABA while increasing the uptake of the excitatory neurotransmitter glutamate.

A-803467 is a selective NaV1.8 channel blocker.